DPC-681

• Description :

  DPC-681 is a potent and selective inhibitor of HIV protease with IC90s for wild-type HIV-1 of 4 to 40 nM. IC50 value: 4 - 40 nM [1] Target: HIV protease in vitro: DPC 681 is extremely potent inhibitor of wild-type HIV-1. When all of the HIV-1 strains tested are considered, the average concentrations required for 90% inhibition of replication were 7.3 ± 3.4 for DPC 681. DPC 681 shows no loss in potency toward recombinant mutant HIVs with the D30N mutation and a fivefold or smaller loss in potency toward mutant variants with three to five amino acid substitutions. [1] in vivo: The total body clearance (CL) of DPC 681 in dogs was high (1.8 liter/h/kg) equaling hepatic blood flow for this species (1.8 liter/h/kg) . After an oral dosing, the Cmax increased ninefold between the 10- and 30-mg/kg DPC 681 dose groups. Bioavailability also increased between the 10- and 30-mg/kg dose groups (18.3 and 78.1%, respectively) . These data suggest that hepatic extraction (first-pass effect) can be saturated in the dog. [1]

• CAS Number :

  [284661-68-3]

• Product Name Alternative :

  DPH-153893

• UNSPSC :

  12352005

• Target :

  HIV; HIV Protease

• Type :

  Reference compound

• Related Pathways :

  Anti-infection; Metabolic Enzyme/Protease

• Applications :

  COVID-19-anti-virus

• Field of Research :

  Infection

• Assay Protocol :

  https://www.medchemexpress.com/DPC-681.html

• Purity :

  99.72

• Solubility :

  DMSO : 100 mg/mL (ultrasonic)

• Smiles :

  O=S(C1=CC(N)=CC=C1)(N(C[C@@H](O)[C@H](CC2=CC=CC=C2)NC([C@H](C(C)(C)C)NC(CNCC3=CC=CC(F)=C3)=O)=O)CC(C)C)=O

• Molecular Formula :

  C35H48FN5O5S

• Molecular Weight :

  669.85

• References & Citations :

  [1]Kaltenbach RF 3rd, et al. DPC 681 and DPC 684: potent, selective inhibitors of human immunodeficiency virus protease active against clinically relevant mutant variants. Antimicrob Agents Chemother. 2001 Nov;45 (11) :3021-8.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 1

• Isoform :

  HIV-1